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PXD007765

PXD007765 is an original dataset announced via ProteomeXchange.

Dataset Summary
TitleDual protein kinase/ nucleoside kinase modulat ors for rationally designed polypharmacology
DescriptionMasitinib, a highly selective protein kinase inhibitor, can sensitise gemcitabine-refractory cancer cell lines when used in combination with gemcitabine. A reverse proteomic approach has identified the target responsible for this sensitisation: the deoxycytidine kinase (dCK). Masitinib, as well as other protein kinase inhibitors such as imatinib, interact with dCK and provoke an unforeseen conformational-dependent activation of this nucleoside kinase, modulating phosphorylation of nucleoside analogue drugs. This phenomenon leads to an increase of prodrug phosphorylation of most of the chemotherapeutic drugs activated by this nucleoside kinase. The unforeseen dual activity of protein kinase inhibition/nucleoside kinase activation could be of great therapeutic benefit, through either reducing toxicity of therapeutic agents by maintaining effectiveness at lower doses or by counteracting drug resistance initiated via down modulation of dCK target.
HostingRepositoryPRIDE
AnnounceDate2024-10-22
AnnouncementXMLSubmission_2024-10-22_04:41:04.033.xml
DigitalObjectIdentifier
ReviewLevelPeer-reviewed dataset
DatasetOriginOriginal dataset
RepositorySupportUnsupported dataset by repository
PrimarySubmitterAUDEBERT Stephane
SpeciesList scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationListmonohydroxylated residue; iodoacetamide derivatized residue
InstrumentLTQ Orbitrap Velos
Dataset History
RevisionDatetimeStatusChangeLog Entry
02017-09-18 02:23:32ID requested
12017-11-13 09:42:14announced
22024-10-22 04:41:08announced2024-10-22: Updated project metadata.
Publication List
Hammam K, Saez-Ayala M, Rebuffet E, Gros L, Lopez S, Hajem B, Humbert M, Baudelet E, Audebert S, Betzi S, Lugari A, Combes S, Letard S, Casteran N, Mansfield C, Moussy A, De Sepulveda P, Morelli X, Dubreuil P, Dual protein kinase and nucleoside kinase modulators for rationally designed polypharmacology. Nat Commun, 8(1):1420(2017) [pubmed]
10.1038/s41467-017-01582-5;
Keyword List
curator keyword: Biomedical
submitter keyword: Human, LTQ-Velos-Orbitrap, labelfree
Contact List
Audebert Stephane
contact affiliationMaP, Marseille Proteomique Centre de Recherche en Cancérologie de Marseille INSERM U1068/Institut Paoli-Calmettes 27, Bd Leï Roure, BP30059, 13273 Marseille CEDEX 9, France
contact emailstephane.audebert@inserm.fr
lab head
AUDEBERT Stephane
contact affiliationMarseille Proteomic, Centre de Recherche en Cancérologie de Marseille, Inserm UMR1068, CNRS UMR7258, Aix Marseille Université U105, Institut Paoli Calmettes, 27 Boulevard Leï Roure CS30059 13273 Marseille Cedex 09 France
contact emailstephane.audebert@inserm.fr
dataset submitter
Full Dataset Link List
Dataset FTP location
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PRIDE project URI
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